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BMS-986142

SKU: orb1302058

Description

BMS-986142 is a potent, selective, and reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM. It is a valuable research tool for studying BTK-dependent signaling in autoimmune and inflammatory disease models, both in cellular assays and in vivo studies.

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

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BMS-986142

Key Properties

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CAS Number1643368-58-4
MW572.6
Purity99.76% (May vary between batches)
FormulaC32H30F2N4O4
SMILESCc1c(cccc1-n1c(=O)n(C)c2c(F)cccc2c1=O)-c1c(F)cc(C(N)=O)c2[nH]c3C[C@H](CCc3c12)C(C)(C)O
TargetBTK
SolubilityH2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.49 mM);DMSO:45 mg/mL (78.59 mM)

Bioactivity

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Target IC50
BLK:23 nM (cell free)|BTK:0.5 nM (cell free)|TXK:28 nM (cell free)|BMX kinase:32 nM (cell free)|TEC:10 nM (cell free)|ITK:15 nM (cell free)
In Vivo
BMS-986142 administration at doses of 4, 10, and 30 mg/kg produces dose-dependent decreases in clinically evident disease by 26%, 43%, and 79%, respectively. Notably, at a 4 mg/kg dose, BMS-986142, when used in conjunction with MTX, enhances clinical scores by achieving a 54% inhibition, compared to a 19% inhibition with MTX alone. Further, this co-administration at 4 mg/kg leads to a 53% reduction in inflammation and bone resorption, significantly more effective than the 24% and 10% reductions observed with each drug individually. Additionally, serum anti-collagen II IgG levels are notably reduced with 10 and 30 mg/kg doses of BMS-986142. The compound also demonstrates efficacy in delayed treatment protocols, showing dose-dependent improvements in clinical scores even when administration begins on day 21, with 2, 4, and 25 mg/kg doses resulting in clinical score reductions of 17%, 37%, and 67%, respectively, by study's end .
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In Vitro
Against a panel of 384 kinases, BMS-986142 is highly selective, with only five other kinases (Tec, ITK, BLK, Txk, BMX) inhibited with <100-fold selectivity for BTK. Four of these kinases are Tec family kinases, of which BTK is a member, and only Tec (IC50: 10 nM) is inhibited with <30-fold selectivity compared with BTK. BMS-986142 does not inhibit CD40L-induced expression of CD86 or CD69 on peripheral blood B cells (IC50>10,000 nM for both). When Ramos B cells are treated with anti-IgM to activate BCR, BMS-986142 inhibits BTK-dependent calcium flux (IC50: 9 nM) .
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Animal Research
Male DBA/1 mice are injected subcutaneously at the base of the tail with bovine type II collagen (200 μg) admixed. The mice are boosted 21 days later in the same manner. For preventative administration, PO QD dosing is immediately started with BMS-986142 in EtOH: TPGS: PEG300 (5:5:90); for therapeutic administration, the start of dosing is delayed until the booster immunization on day 21. For BMS-986142 plus MTX preventative studies, mice receive vehicle; BMS-986142 at 4, 10, or 30 mg/kg; BMS-986142 at 4 mg/kg plus MTX 0.25 mg/kg; or MTX at 0.25 mg/kg daily. For BMS-986142 plus etanercept therapeutic studies, mice receive vehicle daily; BMS-986142 at 2, 4, or 25 mg/kg daily; BMS-986142 at 2 or 4 mg/kg daily plus etanercept at 15 mg/kg IP twice weekly (BIW); or etanercept at 15 mg/kg IP BIW. For BMS-986142 plus murine cytotoxic T lymphocyte-associated protein 4 immunoglobulins (CTLA-4-Ig) preventative studies, mice receive vehicle daily; BMS-986142 at 10 or 30 mg/kg daily; murine CTLA-4-Ig at 0.05 or 0.2 mg/kg IP BIW; or BMS-986142 at 10 mg/kg daily plus murine CTLA-4-Ig at 0.05 or 0.2 mg/kg IP BIW. Dosing proceeds from day 0 through study completion (36 days).
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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BTK, Btk, BMS986142, BMS-986142, Bruton tyrosine kinase, BMS 986142, inhibit, Inhibitor

Similar Products

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  • BMS-986142

    BMS-986142 [orb1226002]

    >98% (HPLC)

    1643368-58-4

    572.613

    C32H30F2N4O4

    1 g, 500 mg, 10 mg, 50 mg, 5 mg, 200 mg, 25 mg, 100 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
86582336 ↗

Key Properties

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No computed properties available.

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BMS-986142 (orb1302058)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 160.00
2 mg
$ 220.00
5 mg
$ 380.00
1 ml x 10 mM (in DMSO)
$ 470.00
10 mg
$ 560.00
25 mg
$ 880.00
50 mg
$ 1,170.00
100 mg
$ 1,520.00
200 mg
$ 2,030.00
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